SKU: T128

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Description
Tenofovir alafenamide is an antiretroviral developed by Gilead and the anti-HIV  activity was reported  in 1993.  It is an investigational precursor to Tenovor, a nucleotide reverse transcriptase inhibitor.  Tenofovir alafenamide is more efficient at delivering Tenofovir to target cells.

    CAS Number

    379270-37-8

    Molecular Formula

    C21H29N6O5P

    Molecular Weight

    476.47

    Mechanism of Action

    Tenofovir alafenamide is a nucleotide analog reverse transcriptase inhibitor that terminates DNA transcription.

    Storage Conditions

    -20C

    Tariff Code

    2933.59.5900

    Spectrum

    antiretroviral

Applications

    Eukaryotic Cell Culture Applications

    Tenofovir alafenamide is 1000- and 10-fold more active against HIV in vitro than Tenofovir or tenofovir disoproxil fumarate, respectively, and the compound is stable in biological matrices (Ray et al, 2016). It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM (Ray et al, 2016). During in vitro studies with activated or resting peripheral blood mononuclear cells, MT2 and Jerkat T-cell lines, authors found that Tenofovir alafenamide did not inhibit mitochondrial DNA synthesis (Stray et al, 2017).

Specifications

    Form

    Powder

    Appearance

    White or off-white powder

    Source

    Synthetic

References

    References

    Balzarini J et al (1993) Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine Antimicrob. Agents Chemother. 37:332-338 PMID 8452366 Lee WA (2005) Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.Antimicrob Agents Chemother. 49(5):1898-1906 PMID 15855512 Ray AS, Fordyce MW, and Hitchcock MJM (2016) Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of human immunodeficiency virus. Antiviral Res. 125:63-70 Stray KM et al (2017) Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human T-cell lines at intracellular concentrations exceeding clinically relevant drug exposures. Antiviral Res. 140:116-120

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